Vandetanib (trifluoroacetate)

Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM) . Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) [1].

Product Specifications

CAS Number

[338992-53-3]

Product Name Alternative

ZD6474 (trifluoroacetate)

UNSPSC

12352005

Target

Apoptosis; Autophagy; VEGFR

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vandetanib-trifluoroacetate.html

Solubility

10 mM in DMSO

Smiles

FC1=CC(Br)=CC=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C23)OC.O=C(O)C(F)(F)F

Molecular Formula

C24H25BrF4N4O4

Molecular Weight

589.38

References & Citations

[1]Wedge SR, et al. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 2002 Aug 15;62 (16) :4645-55.|[2]Hegedus C, et al. Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance. Biochem Pharmacol. 2012 Aug 1;84 (3) :260-7.|[3]Takeda H, et al. Vandetanib is effective in EGFR-mutant lung cancer cells with PTEN deficiency. Exp Cell Res. 2013 Feb 15;319 (4) :417-23.|[4]Inoue K, et al. Vandetanib, an inhibitor of VEGF receptor-2 and EGF receptor, suppresses tumor development and improves prognosis of liver cancer in mice. Clin Cancer Res. 2012 Jul 15;18 (14) :3924-33.